“First-generation” somatostatin receptor agonists (SSTRAs) octreotide and lanreotide are the most commonly used first-line pharmacological therapy for patients with acromegaly. A subset of patients respond only partially or not at all to the first-generation SSTRA, necessitating the use of additional pharmacological agents or other modes of therapy. Pasireotide is a “second-generation” SSTRA that has multi-receptor activity. Prospective studies have shown promise in the use of pasireotide in patients with poor response to first-generation SSTRA. Here we elucidate the molecular pathways of resistance to first-generation SSTRA, the mechanism of action, pre-clinical and clinical evidence of the use of pasireotide in patients having incomplete / lack of response to first-generation SSTRA. We also discuss the clinical, pathological, and radiological markers predicting response to pasireotide, and the difference in side-effect profiles of pasireotide, compared to first-generation SSTRA.

“第一代”生长抑素受体激动剂（SSTRA）奥曲肽和兰瑞肽是肢端肥大症患者最常用的一线药物治疗。一部分患者对第一代 SSTRA 仅部分反应或根本没有反应，需要使用额外的药物或其他治疗方式。帕瑞肽是“第二代”SSTRA，具有多受体活性。前瞻性研究表明，帕瑞肽治疗对第一代 SSTRA 反应不佳的患者有希望。在这里，我们阐明了第一代 SSTRA 耐药的分子途径、作用机制、帕瑞肽在对第一代 SSTRA 不完全/缺乏反应的患者中使用的临床前和临床证据。我们还讨论了预测帕瑞肽反应的临床、病理和放射学标志物，以及帕瑞肽与第一代 SSTRA 相比副作用特征的差异。